PF-05212377 (SAM-760; WYE-103760) is an orally available, high-affinity, selective 5-hydroxytryptamine (5-HT; serotonin) receptor 5-HT6 antagonist (Ki/IC50 = 0.53/1.06 nM against 3 nM [3H]-LSD for binding human 5-HT6). PF-05212377 modulates glutamate and acetylcholine release in the cerebral cortex and hippocampus in rodents with in vivo pro-cognitive efficacy.
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